| 货号 | 3368/50 |
| 别名 | 5-Chloro-N-[4-methoxy-3-(1-piperazi |
| 供应商 | Tocris |
| 生物活性 | Selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F,α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM). |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >99 % |
| 计算分子量 | 488.45 |
| 分子式 | C20H22CIN3O3S2.HCl |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| CAS号 | 209481-20-9 |
| 参考文献 | Marcoset al (2008) Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br.J.Pharmacol. 155 434. PMID: 18622410. Dawsonet al(2000)In vivo effects of the 5-HT6 antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartate. Br.J.Pharmacol. 130 23. PMID: 10780993. Routledgeet al (2000) Characterization of SB-271046: a potent, selective and orally active 5-HT6 receptor antagonist. Br.J.Pharmacol. 130 1606. PMID: 10928964. Bromidgeet al (1999) 5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J.Med.Chem. 42 202. PMID: 9925723. |